this compound was initially developed by a team at upjohn in the 1970s. upjohn created over a dozen patents on related compounds until they discovered that u-47700 was the most active. this was done by looking for the key functional groups which gave the greatest activity.
very little is known about the toxicity of u-47700 and it has very little history of human usage. it is currently available as a gray-area research chemical distributed by online vendors. many reports suggest that it possesses unique physical properties relative to most opioids such as an unusual amount of causticity (ability to destroy living tissue) that may make it significantly more harmful to expose to the body, particularly when it is injected. it is strongly advised to use harm reduction practices if choosing to use this substance.
u-47700 is an atypical opioid of the benzamide class. it features core phenyl ring with two chlorine atoms at carbons r3 and r4. this ring is connected to an amine group through a carboxyl group (c=o). the terminal nitrogen atom of the amide group is bonded to a methyl carbon and substituted cyclohexane ring. the cyclohexane ring is further substituted at r2 with a dimethylamino group, thus forming the structure of u-47700.
u-47700 is selective for the µ-opioid receptor, with various sources claiming 7.5x the potency of morphine.
opioids exert their effects by binding to and activating the μ-opioid receptor. this occurs because opioids structurally mimic endogenous endorphins which are naturally found in the body and also work with the μ-opioid receptor set. the way in which opioids structurally mimic these natural endorphins results in their euphoria, pain relief and anxiolytic effects. this is because endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. they can be released in response to pain, strenuous exercise, orgasm, or general excitement.
u-47700 may also be an agonist for the kappa-opioid receptor system. as a result of this, it has become the lead compound of selective kappa-opioid receptor ligands such as u-50488 and u-69,593, which share very similar structures. its structure led to other chemists experimenting with it to see if rigid analogs would retain activity. although not used medically, the selective kappa ligands are used in research.